染料木素MePEG-PLGA共聚物胶束体内外抗肿瘤作用

目的 探讨染料木素MePEG-PLGA共聚物胶束对人肝癌SMMC-7721细胞的体内外抗肿瘤作用。方法 采用MTT法、Annexin V-FITC/PI染法分别考察染料木素MePEG-PLGA共聚物胶束对人肝癌SMMC-7721细胞的细胞毒性、细胞凋亡、细胞周期的影响；通过荷肝SMMC-7721瘤裸鼠体内抗肿瘤试验，考察染料木素胶束的体内抗肿瘤效应。结果 染料木素胶束对肝癌SMMC-7721细胞的抑制率均高于染料木素，最高抑制率分别可达83.26%，78.25%。流式细胞仪检测结果显示，染料木素胶束组能够提高染料木素对SMMC-7721细胞凋亡的诱导能力，并且呈浓度依赖性。5，10，20 μg·mL^-1的染料木素组和染料木素胶束组药物作用于SMMC-7721细胞48 h时，染料木素胶束能够明显提高染料木素对细胞G₂/M期细胞的阻滞作用，并且呈现浓度依赖性。体内抗肿瘤试验结果表明，相同浓度的染料木素胶束组的抑瘤效果显著强于染料木素乳剂组，呈浓度依赖性，最高抑瘤率可达55.41%。结论 染料木素MePEG-PLGA共聚物胶束在体内和体外均有显著的抗肝癌作用。

Anti-tumor Effect of Genistein MePEG-PLGA Copolymer Micelles in vitro and in vivo

OBJECTIVE To study the anti-tumor effect of genistein(GEN) MePEG-PLGA copolymer micelles on human hepatoma SMMC-7721 cells in vitro and in vivo. METHODS MTT assay, Annexin V-FITC/PI staining were used to investigate the effects of GEN MePEG-PLGA copolymer micelles on cytotoxicity, apoptosis and cell cycle of human hepatoma SMMC-7721 cells. The in vivo anti-tumor effect of GEN micelles was investigated in nude mice bearing hepatocellular carcinoma SMMC-7721 tumor in vivo. RESULTS The inhibitory rate of GEN micelles in SMMC-7721 cells were higher than GEN and the highest inhibition rates were 83.26% and 78.25%, respectively. The results of flow cytometry showed that the GEN micelles group could increase the ability of GEN to induce apoptosis of SMMC-7721 cells and presented a concentrationdependent manner. When the concentration of 5, 10, 20 μg·mL^-1 GEN and GEN micelles groups acted on SMMC-7721 cells for 48 h, the GEN micelles could significantly enhance the ability of arrest cell in G₂/M phase for GEN, and showing a concentration-dependent manner. In vivo anti-solid tumor experimental results showed that the same concentration of GEN micelles group had significantly better anti-tumor effect than GEN emulsion, and in a concentration-dependent manner, the highest tumor inhibition rate was 55.41%. CONCLUSION The GEN MePEG-PLGA copolymer micelles has significant anti-hepatocarcinoma effects both in vivo and in vitro.